Department of Chemical Sciences National Institute of Pharmaceutical Education and Research (NIPER) Hyderabad 500 037 Telangana State India
Division of Molecular Microbiology and Immunology CSIR-Central Drug Research Institute (CDRI) Sitapur Road, Sector 10, Janakipuram Extension Lucknow 226 031 Uttar Pradesh India
AcSIR: Academy of Scientific and Innovative Research (AcSIR) Ghaziabad 201 002 India
合成了多种 3,4-dihydro-1 H - benzo[ b ]azepine-2,5-dione 衍生物，并针对一组细菌病原体进行了筛选。在测试中。化合物16 d、16 f和16 g对金黄色葡萄球菌 ATCC 29213表现出良好的抑制作用（MIC 4 μg/mL），16 a、16 e、16 f、16 g和16 i表现出对Mtb H37Rv的有效抑制作用（MIC 2- 4 μg/mL）具有良好的选择性指数（SI≥10）。此外，16 f表现出对鲍曼不动杆菌 BAA-1605 的有效抑制作用(MIC 2 微克/毫升)。SAR 研究揭示了 4-((2-phenylhydrazineyl)methylene)-3,4-dihydro-1 H - benzo[ b ]azepine-2,5-diones core 对于有希望的抗菌性能的重要性。
"点击查看英文标题和摘要"
Synthesis and Antibacterial Evaluation of 3,4-Dihydro-1H-benzo[b]azepine-2,5-dione Derivatives
Diverse 3,4-dihydro-1H-benzo[b]azepine-2,5-dione derivatives were synthesized and screened against a panel of bacterial pathogens. Among the tested. Compounds 16 d, 16 f and 16 g showed good inhibition against S. aureus ATCC 29213 (MIC 4 μg/mL), 16 a, 16 e, 16 f, 16 g and 16 i exhibited potent inhibition against Mtb H37Rv (MIC 2-4 μg/mL) with good selectivity index (SI≥10). In addition, 16 f demonstrated potent inhibition against A. Baumannii BAA-1605 (MIC 2 μg/mL). SAR studies revealed importance of 4-((2-phenylhydrazineyl)methylene)-3,4-dihydro-1H-benzo[b]azepine-2,5-diones core for promising antibacterial properties.
京公网安备 11010802027423号